Polr2j Inhibitors
Chemical inhibitors of Polr2j employ various mechanisms to impede the protein's function within the RNA polymerase II complex. α-Amanitin binds with high affinity to the RNA polymerase II, effectively blocking the enzyme's progression along the DNA template, thereby preventing Polr2j from fulfilling its role in the transcription process. Similarly, Triptolide targets the complex by covalently modifying a cysteine residue in RNA polymerase II, leading to its degradation. This action results in a decrease in the functional presence of Polr2j within the cell. DRB operates by inhibiting the phosphorylation of the C-terminal domain of RNA polymerase II, a critical step for transcription elongation, indirectly impeding Polr2j activity. Actinomycin D disrupts transcription by intercalating into DNA, which prevents the RNA polymerase II from elongating RNA chains and thus inhibits Polr2j function.
In addition to the direct inhibitors of transcription, several chemicals interfere with Polr2j function by targeting associated processes. Cordycepin incorporates into RNA chains and causes premature termination of RNA synthesis, which affects Polr2j's role in RNA chain elongation. ICRF-193 and Meayamycin disrupt DNA replication and RNA splicing, respectively, processes that are closely linked with Polr2j's function in transcription. Pladienolide B targets the spliceosome, a complex intimately involved with RNA polymerase II during transcription, thereby indirectly affecting Polr2j. Amiloride and CBR-5884 influence the cellular environment and metabolic pathways, leading to an indirect modulation of Polr2j functionality. Lastly, Cantharidin inhibits protein phosphatases, altering the phosphorylation state of proteins related to RNA polymerase II and thus influencing Polr2j's activity.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $269.00 $1050.00 | 26 | |
α-Amanitin is a potent inhibitor of RNA polymerase II, the enzyme for which Polr2j is a subunit. By binding strongly to RNA polymerase II, α-Amanitin blocks the translocation of the enzyme along the DNA, thus directly inhibiting the functionality of Polr2j within the larger RNA polymerase complex. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide is a diterpene triepoxide that has been shown to covalently modify a cysteine residue in the largest subunit of RNA polymerase II, leading to the degradation of RNA polymerase II and consequent functional inhibition of Polr2j as part of the polymerase complex. | ||||||
DRB | 53-85-0 | sc-200581 sc-200581A sc-200581B sc-200581C | 10 mg 50 mg 100 mg 250 mg | $43.00 $189.00 $316.00 $663.00 | 6 | |
DRB acts as an inhibitor of RNA polymerase II transcription elongation. By inhibiting the phosphorylation of the RNA polymerase II C-terminal domain, DRB indirectly impedes the function of Polr2j as it is reliant on the proper assembly and phosphorylation of the polymerase complex for its activity. | ||||||
Actinomycin D | 50-76-0 | sc-200906 sc-200906A sc-200906B sc-200906C sc-200906D | 5 mg 25 mg 100 mg 1 g 10 g | $74.00 $243.00 $731.00 $2572.00 $21848.00 | 53 | |
Actinomycin D intercalates into DNA at the transcription initiation complex, preventing RNA polymerase II from elongating RNA chains. This binding action leads to inhibition of Polr2j function as it is unable to participate in the transcription process without RNA chain elongation. | ||||||
Cordycepin | 73-03-0 | sc-203902 | 10 mg | $101.00 | 5 | |
Cordycepin is an adenosine analog that terminates RNA synthesis prematurely by being incorporated into the growing RNA chain and inhibiting RNA polymerase II, thereby functionally inhibiting the role of Polr2j in the RNA synthesis process. | ||||||
ICRF-193 | 21416-68-2 | sc-200889 sc-200889A | 1 mg 5 mg | $341.00 $927.00 | 7 | |
ICRF-193 is a bisdioxopiperazine that interferes with the DNA topoisomerase II, creating a stable cleavable complex and thereby preventing DNA replication and transcription. This indirectly inhibits Polr2j by hindering the transcription process that it is a part of. | ||||||
Pladienolide B | 445493-23-2 | sc-391691 sc-391691B sc-391691A sc-391691C sc-391691D sc-391691E | 0.5 mg 10 mg 20 mg 50 mg 100 mg 5 mg | $299.00 $5699.00 $11099.00 $25500.00 $66300.00 $2875.00 | 63 | |
Pladienolide B is a substance that binds to the spliceosome and inhibits its function. Since the splicing of pre-mRNA is tightly coupled with transcription by RNA polymerase II, this inhibition can disrupt the transcriptional activity in which Polr2j is involved. | ||||||
Amiloride | 2609-46-3 | sc-337527 | 1 g | $296.00 | 7 | |
Amiloride, primarily known as a potassium-sparing diuretic, also inhibits certain isoforms of the sodium/hydrogen antiporter (NHE). By altering intracellular pH, it can indirectly affect the functionality of proteins, including Polr2j, by modulating the cellular environment necessary for its activity. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin inhibits protein phosphatases 1 and 2A, which are involved in numerous cellular processes, including the regulation of transcription factors and other proteins associated with RNA polymerase II function, therefore indirectly inhibiting Polr2j by altering its phosphorylation state. | ||||||